Nanoemulsion eyedrop composition containing cyclosporine and method for preparing same

A technology of cyclosporine and composition, applied in the field of nanoemulsion eye drop composition containing cyclosporine and its preparation, can solve the problems of large manufacturing equipment, difficulty in ensuring consistent quality of preparation batches, and acceleration of emulsion separation. layer process etc.

Active Publication Date: 2016-02-03
TAEJOON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As disclosed in Korean Patent Laid-Open No. 10-2008-0030828, this production method requires a large manufacturing facility and huge expenditure, and is difficult to apply to thermal Sensitive ingredients
In addition, cyclosporine emulsions prepared by this method flocculate rapidly due to different oil droplet sizes, and thus accelerate the emulsion separation process and affect the long-term stability
In addition, due to the relatively broad particle size distribution in the dispersed phase, it is difficult to ensure consistent quality from batch to batch

Method used

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  • Nanoemulsion eyedrop composition containing cyclosporine and method for preparing same
  • Nanoemulsion eyedrop composition containing cyclosporine and method for preparing same
  • Nanoemulsion eyedrop composition containing cyclosporine and method for preparing same

Examples

Experimental program
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Effect test

experiment Embodiment 1

[0068] Experimental example 1. prepare nanoemulsion according to the type and content variation of non-aqueous solvent and measure its average particle size

[0069] Nanoemulsion compositions were prepared with different amounts of castor oil, labrafac lipophilic WL1349 or miglyol812, and then their average particle size was measured. The specific method for preparing the nanoemulsion composition is as follows. At 600rpm to 800rpm and 70°C, by using a stirrer (Super-Nuova TM Multi-place, ThermoScientific) Cyclosporine A was mixed with non-aqueous solvent in the amount shown in Table 1 below and completely dissolved. An oil phase was prepared by adding the hydrophilic and hydrophobic emulsifiers in the amounts shown in Table 1 to the mixed solution prepared above and mixing it thoroughly by stirring it. The prepared solution was cooled at room temperature, and the oil phase was placed into an aqueous solvent to wash the oil phase several times, then at 400-500rpm and at room ...

experiment Embodiment 2

[0072] Experimental Example 2. Preparation of nanoemulsions and measurement of their average particle size according to the type and varying amount of emulsifiers

Embodiment 1

[0073] The nanoemulsion compositions of Examples 16-36 were prepared by the same method described in Experimental Example 1 by using castor oil as the non-aqueous solvent, and varying the amount of castor oil and the type and amount of emulsifier. The compositions and amounts of the prepared nanoemulsion compositions are shown in Table 2 below.

[0074]

[0075] As shown in Table 2, it was confirmed that in Examples 16-34, the average particle size of the nanoemulsion composition was 100 nm or less, and its particle size distribution was very narrow. Therefore, it was confirmed that when cyclosporine, castor oil, hydrophilic emulsifier, hydrophobic emulsifier, and aqueous solvent were mixed in the above composition, an ophthalmic nanoemulsion having an average particle size of 100 nm or less and a narrow particle size distribution could be prepared combination.

[0076] In Table 2, Example 35 and Example 36 are compositions prepared by using only hydrophilic emulsifiers with...

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Abstract

The present invention relates to a nanoemulsion eyedrop composition and a method for preparing the same which increases the solubility of cyclosporine as an active ingredient and improves the stability of the eyedrop composition by mixing cyclosporine, a nonaqueous solvent, an emulsifier, and an aqueous solvent, and a method for preventing or treating dry eye syndrome using the same. The nanoemulsion eyedrop composition according to the present invention is characterized by having an average particle size of 200 nm or less, preferably 100 nm or less, and having a very narrow particle distribution. Therefore, the composition enables sterilizing filtration, improves stability, and has an excellent effect of clinically improving foreign body sensation and blurred vision, and thus can be effectively used for ophthalmic administration.

Description

technical field [0001] The present disclosure relates to ophthalmic nanoemulsion compositions and methods of making them by mixing cyclosporin, a non-aqueous solvent, an emulsifier, and an aqueous solvent to increase the solubility of cyclosporine as an active ingredient and improve the ophthalmic properties. Compositions) and methods of using same to prevent or treat eye diseases. Background technique [0002] Immunosuppressive drugs are drugs used in immunosuppressive therapy by preventing or suppressing abnormal immune reactivity. Immunosuppressive drugs are currently used in a variety of diseases (including transplant rejection after organ and tissue transplantation; inflammatory bowel disease, such as ulcerative colitis or Crohn's disease; rheumatoid arthritis; Behcet's syndrome; Inflammatory or allergic skin disease such as psoriasis or atopic dermatitis; inflammatory or allergic respiratory disease such as chronic obstructive pulmonary disease or asthma; systemic lup...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K9/08A61P27/02
CPCA61K9/0048A61K9/1075A61K38/13A61K47/08A61K47/10A61K47/14A61K47/26A61K47/44A61P27/02A61K9/08A61K9/113A61K47/30
Inventor 李俊晔慎允宰柳尚录
Owner TAEJOON PHARMA
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